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GSK2239633A

目录号: PL01032 纯度: ≥99%

GSK2239633A 是一种 CC 趋化因子受体4 (CCR4) 拮抗剂，抑制 [¹²⁵I]-TARC 与人 CCR4 结合，pIC50 为 7.96±0.11。

CAS No. :1240516-71-5

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中文名称	GSK2239633A
英文名称	GSK2239633A
英文别名	GSK2239633A;GSK 2239633A;07ODS257BP;N-[[3-[[3-[(5-chlorothiophen-2-yl)sulfonylamino]-4-methoxyindazol-1-yl]methyl]phenyl]methyl]-2-hydroxy-2-methylpropanamide;N-[[3-[[3-[[(5-Chloro-2-thienyl)sulfonyl]amino]-4-methoxy-1H-indazol-1-yl]methyl]phenyl]methyl]-2-hydroxy-2-methylpropanamide;GTPL10416;BCP29621;BDBM50380880;compound 6 [PMID: 23409871];Q27895967;N-((3-((3-((5-Chloro-2-thienyl)sulfonylamino)-4-methoxy-indazol-1-yl)methyl)phenyl)methyl)-2-hydroxy
Cas No.	1240516-71-5
分子式	C₂₄H₂₅ClN₄O₅S₂
分子量	549.06
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	GSK2239633A 是一种 CC 趋化因子受体4 (CCR4) 拮抗剂，抑制 [¹²⁵I]-TARC 与人 CCR4 结合，pIC50 为 7.96±0.11。

产品详情	GSK2239633A 是一种 CC 趋化因子受体4 (CCR4) 拮抗剂，抑制 [¹²⁵I]-TARC 与人 CCR4 结合，pIC₅₀ 为 7.96±0.11。
生物活性	GSK2239633A is a CC-chemokine receptor 4 (CCR4) antagonist, which inhibits the binding of [I]-TARC to human CCR4 with a pIC 50 of 7.96?±?0.11.
性状	Solid
IC50 & Target[1][2]	[I]-TARC-CCR4 7.96 (pIC50)
体外研究(In Vitro)	The GSK2239633A is an allosteric antagonist of human CCR4. GSK2239633A inhibits the binding of [I]-TARC to human CCR4 with a pIC50 of 7.96±0.11 and also inhibits thymus- and activation-regulated chemokine-induced (TARC)-induced increases in the F-actin content of isolated human CD4 CCR4 T-cells with a pA2 of 7.11±0.29. The effect of GSK2239633A (Compound 3) on CCL17-induced increases in the F-actin content of human CD4 CCR4 T cells is measured. The pEC50 value is 8.79±0.22. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	Following intravenous dosing, plasma GSK2239633A displays rapid, bi-phasic distribution and slow terminal elimination (t 1/2 : 13.5 hours), suggesting that GSK2239633A is a low to moderate clearance drug. Following oral dosing, blood levels of GSK2239633A reach C max rapidly (median t max : 1.0-1.5 hours). Estimated GSK2239633A bioavailability is low with a maximum value determined of only 16%. GSK2239633A (Compound 9) demonstrates good pharmacokinetic data in preclinical animal studies (bioavailability in rats and beagle dogs 85% and 97% respectively). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Cahn A, et al. Safety, tolerability, pharmacokinetics and pharmacodynamics of GSK2239633, a CC-chemokine receptor 4 antagonist, in healthy male subjects: results from an open-label and from a randomised study. BMC Pharmacol Toxicol. 2013 Feb 28;14:14. [2]. Slack RJ, et al. Antagonism of human CC-chemokine receptor 4 can be achieved through three distinct binding sites on the receptor. Pharmacol Res Perspect. 2013 Dec;1(2):e00019.

溶解度数据	In Vitro: DMSO : ≥ 250 mg/mL (455.32 mM)配制储备液

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[1]. Cahn A, et al. Safety, tolerability, pharmacokinetics and pharmacodynamics of GSK2239633, a CC-chemokine receptor 4 antagonist, in healthy male subjects: results from an open-label and from a randomised study. BMC Pharmacol Toxicol. 2013 Feb 28;14:14.
[2]. Slack RJ, et al. Antagonism of human CC-chemokine receptor 4 can be achieved through three distinct binding sites on the receptor. Pharmacol Res Perspect. 2013 Dec;1(2):e00019.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

GSK2239633A

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